Background: The current research focused on the improvement of drug entrapment efficiency and release study of hydrophilic drug through polymer complextation Objective: Ionotropic gelation technique was utilised for the preparation of Polyelectrolyte complex microbeads of Vildagliptin using Sodium alginate and Eudragit RL100 and their performance was optimized by Central composite design. Method: Fourier Transform Infrared Spectroscopy, Scanning Electron Microscope, Differential Scanning Calorimetry, particle size, Drug Entrapment Efficiency, X-ray diffraction and in-vitro drug release at 10hr were chosen for evaluating formulated microbeads. The impact of independent variables like concentration of sodium alginate and eudragit RL100 was examined over dependent responses. Result: The interpretation of XRD, SEM, DSC, and FTIR affirmed no drug excipients interference and confirmed formation of polyelectrolyte complex microbeads. For complex microbeads, the maximum and minimum drug release after 10 hours was obtained as 96.23.5% and 89.45%, respectively. The 32 central composite design was further used to obtain response surface graph and the values for the particle size, DEE and Drug release were retained as 0.197, 76.30 % and 92.15%, respectively for the optimize batch. Conclusion: The result suggested the combination of two polymers (Sodium alginate and Eudragit RL100) were suitable for improving the entrapment efficiency of hydrophilic drug (Vildagliptin). The central composite design (CCD) technique is an effective tool for obtaining optimal drug delivery systems of Vildagliptin polyelectrolyte complex microbeads.

Background: This study aims to formulate and characterize sorafenib-loaded resealed erythrocytes (SoRE) and investigate their anticancer activity in a rat model of hepatocellular carcinoma. Methods: SoRE were prepared by hypotonic dialysis of red blood cells obtained from Wistar rats using a range of drug-containing dialysis mediums (2-10 mg/ml) and osmosis time (30-240 mins). Optimized SoRE (8 mg/mL and 240 mins) were characterized for size, morphology, stability, entrapment efficiency, in-vitro release profiles, and in-vivo efficacy evaluations. For efficacy studies, optimized SoRE were intravenously administered to Wistar rats having hepatocellular lesions induced by aflatoxin B and monitored for in-vivo antineoplastic activity. Results: The amount of sorafenib entrapped was directly proportional to the drug concentration in the dialysis medium and duration of osmosis; highest for 10 mg/mL and 240 minutes and lowest for 2 mg/mL and 30 minutes, respectively. Optimized SoRE were biconcave with a size of 112.7 nm and zeta potential of -11.95  2.25 mV. Osmotic and turbulence fragility were comparable with native erythrocytes. Conclusion: Drug release follows the first-order pattern. In-vivo investigations reveal better anticancer activity of SoRE formulation compared to sorafenib standard preparation. Resealed erythrocytes loaded with sorafenib displayed first-order in-vitro release and promising anticancer activity in a rat model of hepatocellular carcinoma.

Background: Darifenacin hydrobromide, a BCS Class II drug, is poorly bioavailable due to extensive first-pass metabolism. The present study is an attempt to investigate an alternative route of drug delivery by developing a nanometric microemulsion-based transdermal gel for the management of an overactive bladder. Method: Oil, surfactant, and cosurfactant were selected based on the solubility of the drug, and surfactant: cosurfactant in surfactant mixture (Smix) was selected at a 1:1 ratio as inferred from the pseudo ternary phase diagram. The D-optimal mixture design was used to optimize the o/w microemulsion wherein the globule size and zeta potential were selected as dependable variables. The prepared microemulsions were also characterized for various physico-chemical properties like transmittance, conductivity, and TEM. The optimized microemulsion was gelled using Carbopol 934 P and assessed for drug release in-vitro and ex-vivo, viscosity, spreadability, pH, etc. Results: Drug excipient compatibility studies showed that the drug was compatible with formulation components. The optimized microemulsion showed a globule size of less than 50 nm and a high zeta potential of -20.56 mV. The ME gel could sustain the drug release for 8 hours as reflected in in-vitro and ex-vivo skin permeation and retention studies. The accelerated stability study showed no significant change in applied storage conditions. Conclusion: An effective, stable, non-invasive microemulsion gel containing darifenacin hydrobromide was developed. The achieved merits could translate into increased bioavailability and dose reduction. Further confirmatory in-vivo studies on this novel formulation, which is a cost-effective & industrially scalable option, can improve the pharmacoeconomics of overactive bladder management.

The discovery of proteins and peptides marked the actual beginning for pharmaceutical companies to do research on novel delivery systems for delivering these therapeutic proteins. Biodegradable polymer-based microspheres for controlled-release depot injection are known for decades and have proved to be one of the best possible approaches. Despite being known for decades, the commercial success of microsphere-based delivery systems remains limited. Very few products are seen in the market with no generics available for approved brand products whose patents have either expired or are about to expire. This all points to the complexities involved in developing these delivery systems. Still, many hurdles remain in developing these drug delivery systems namely, poor drug entrapment, unwanted burst release, poor in vitro in vivo correlation, lack of proper in vitro testing methods, problems involved during scale-up, and the most important hurdle being sterilization of the product. To achieve successful product development, all of these technical difficulties need to be simultaneously dealt with and resolved. This article attempts to highlight the problem areas for these delivery systems along with the regulatory requirements involved and map the present status of these delivery systems.

The majority of drugs taken orally have limited aqueous solubility and dissolution rate. Cyclodextrin (CD) and its derivatives are used as pharmaceutical adjuvants, contributing to the development of safe and high bioavailability formulations. CDs have a unique structure with a variety of physicochemical features that aid pharmaceutical scientists in solving drug delivery issues for poorly water-soluble drugs (PWS). This article covers information about cyclodextrin and its various derivatives, its different manufacturing process, physicochemical properties, advantages, and recent advancements. There are various advantages of CD-based inclusion complexes, such as enhancement of solubility, bioavailability, and stability and reduction of irritation caused by the drug. Moreover, they are used as odor and taste enhancers and also prevent incompatibility by physically isolating the incompatible drug components in drug formulation. CD and its derivatives are extensively employed as solubilizers in the manufacturing of parenteral and oral dosage forms. Inclusion complexes formed by CDs with appropriately sized guest molecules improve drug water solubility, physical-chemical stability, and bioavailability. Simultaneously CDs prevent the drugs from degradation like oxidation, hydrolysis, and photodegradation and extend the shelf life of the drug. The manuscript also highlights patents and exclusive branded formulations of modified CDs. It also discusses the different examples of chemically modified CDs, i.e., captisol, sulfobutyl ether-β-CD, hydroxy propyl betadex, randomly methylated β-CD, methyl β-CD, and hydoxy propyl γ-CD, all are used in the various dosage forms.

Deep eutectic solvents (DESs) containing bioactive have been explored as potential choices for therapeutic efficiency enhancement. DESs are regarded as superior compared to established solvents owing to accessibility, storage conditions, synthesis, and low cost. As such, intensive research has taken place in different disciplines, especially nutraceuticals, foods and pharmaceuticals. The applications of DESs, especially in nutraceuticals and pharmaceutical delivery, have shown great promise. Despite these different successes, the safety issues of these DESs need to be properly identified. A safe mixture of DESs must be developed to take its broad range of advantages to the nutraceutical industry, and, therefore, its nutraceutical applications can only be introduced if DESs are known to have profiles of negligible or minimal toxicity. This review emphasizes the fundamental aspects needed to have a better understanding of DESs. It covers the current prospects of DES, including types, properties, formulation components and characterization methods. The several characterization methods, viz., pH, density, refractive index, viscosity, surface tension, solubility, polarized optical microscopy, x-ray diffraction studies, Fourier transforms infrared spectroscopy, and Nuclear magnetic resonance spectroscopy are also mentioned. Further, the promising applications of DESs in different nutraceutical and pharmaceutical domains are highlighted.

Aim and Objective The primary aim of the present investigation was to adopt the concept of quality by design (QbD) for developing Febuxostat matrix tablets containing a novel combination of polyethylene oxide (PEO), pre-gelatinized starch (PGS) and lactose for obtaining biphasic drug release. Experimental work Febuxostat-containing matrix tablets were prepared by direct compression using 32 full factorial designs. The tablets were prepared with varying amounts of PEO WSR 301 to PGS and lactose to obtain the desired release pattern. The chosen responses were cumulative % drug released at 1, 6 and 12 hours. The evaluation of tablets was done for pre and post-compressional parameters. Compared with the marketed tablet, the optimized formulations were selected based on in vitro drug release. Dose dumping was checked in the dissolution medium containing up to 40% alcohol. Result and discussion The results of the dissolution study indicated that the batch containing a 1:1 ratio of PEO WSR 301 and PGS (15 mg each) and 20 mg of Lactose showed fast initial drug release to imitate the pharmacological action followed by sustained drug release effect. The use of Lactose facilitated immediate drug release, while PEO WSR 301 and PGS exhibited the opposite effect on cumulative drug release. The results of the 32 Factorial design revealed that the concentration of Lactose is a critical parameter. Dose dumping was not observed in the alcoholic dissolution medium. Kinetic equations were fitted to the dissolution data after 1 hour of the dissolution study. Conclusion The type (soluble or swellable) and the concentration of excipients (low or high) dictate the tablets' drug release. The study's outcome revealed that the most critical material attribute is the amount of lactose. The novel combination of PEO, PGS and lactose can bypass existing patents and give more industrial applicability.